Chronic Disease and Inflammation

Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used clinically to treat type 2 diabetes mellitus.

Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.

Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.

Ligustrazine (Chuanxiongzine) is an orally active, blood-brain barrier-permeable alkaloid. It can be isolated from Ligusticum striatum DC. Ligustrazine reduces ROS, upregulates the levels of p-Akt/Akt and p-eNOS/eNOS, and decreases ALT and AST. It inhibits glutamate excitotoxicity, calcium overload, oxidative stress, ischemia-reperfusion injury and atherosclerotic plaque progression, enhances synaptic plasticity, and improves neurological function, cerebral infarct volume and brain water content. Ligustrazine possesses anti-inflammatory, antioxidant, lipid-lowering, endothelial protective and hepatoprotective activities. It can be used in studies related to ischemic stroke, cerebral ischemia-reperfusion injury and atherosclerosis.

DSPE-PEG2000-DBCO is a phospholipid PEG polymer that combines a hydrophobic phospholipid (DSPE), a hydrophilic polyethylene glycol spacer with a molecular weight of 1000 Da, and a reactive click chemistry terminal group (DBCO). DSPE-PEG2000-DBCO migrates to lymph nodes via the endogenous albumin transport system, implants bioorthogonal DBCO docking sites, and enables the enrichment of azide-functionalized vesicles in lymph nodes mediated by click chemistry. DSPE-PEG2000-DBCO can be used in studies related to atherosclerosis.

Acetazolamide sodium is a carbonic anhydrase (CA) IX inhibitor with an IC₅₀ of 30 nM for hCA IX. Acetazolamide sodium has diuretic, antihypertensive and anti-gonococcal activities.

2-Methylbutyrylcarnitine (2MBC) is an orally active short-chain branched-chain acylcarnitine and a gut microbiota co-metabolite produced from 2-methylbutyric acid via branched-chain amino acid catabolism. 2-Methylbutyrylcarnitine activates platelet integrin α2β1 (K_d = 10.6 μM), initiates the downstream p38‑cPLA2 signaling cascade, elevates TXA2 production, and thereby enhances platelet hyperreactivity. 2-Methylbutyrylcarnitine can be used in research on atherosclerosis and thrombosis.

PXS-4728A is an orally active, selective VAP-1/SSAO inhibitor with an IC₅₀ of 5 nM and a K_i of 175 nM. PXS-4728A inhibits the expression of MMP-9. It reduces cell rolling, adhesion and migration, decreases cell infiltration levels, pro-inflammatory cytokines, chemokines and collagen deposition, and improves pulmonary function. PXS-4728A reduces the formation and progression of atherosclerotic plaques, and decreases blood lipid and blood glucose levels as well as body weight gain. PXS-4728A can be used in research related to chronic obstructive pulmonary disease, cystic fibrosis, acute pulmonary inflammation, acute lung injury, bronchiolitis obliterans syndrome, rhinovirus-exacerbated asthma, sepsis, Klebsiella pneumoniae pulmonary infection and atherosclerosis.

Cholestyramine (Cholestyramine resin) is an orally active bile acid sequestrant. Cholestyramine upregulates the expression of intestinal Apical sodium-dependent bile acid transporter and hepatic Cholesterol 7α-hydroxylase. Cholestyramine induces the expression of intestinal and hepatic cholesterol synthesis genes as well as hepatic lipogenesis genes, and promotes bile acid- and neutral sterol-mediated reverse cholesterol transport. Cholestyramine reduces intestinal cholesterol absorption and induces cholesterol efflux. Cholestyramine is applicable to research related to coronary artery disease, atherosclerotic cardiovascular disease and atherosclerosis.

PPACK TFA is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK TFA specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK TFA exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK TFA binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK TFA is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.

Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma.

Basiliximab (CHI 621) is a recombinant chimeric murine/human IgG1 monoclonal anti-interleukin-2 receptor antibody. Basiliximab can be used for the research of renal transplantation.

Verekitug (ASP-7266; TRAB-1; UPB-101) is a human monoclonal antibody targeting the thymic stromal lymphopoietin receptor (TSLPR), with a mean half-life of approximately 20 days. At doses of Verekitug ≥100 mg, complete and sustained TSLPR-specific occupancy is achieved, and the antibody does not bind to IL-7Rα. By inhibiting TSLP-driven inflammatory responses, Verekitug blocks TSLP-induced cell proliferation and TARC expression, while reducing fractional exhaled NO levels, blood eosinophil counts, and levels of IL-5 and IgE. Verekitug significantly improves scores for nasal polyps, nasal congestion and olfactory dysfunction, with favorable safety and good tolerability; potential adverse reactions include headache, upper respiratory tract infection, sinusitis and nasopharyngitis. Verekitug is used in relevant studies on asthma, chronic rhinosinusitis with nasal polyps and chronic obstructive pulmonary disease.

Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.

Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.

Acyl coenzyme A synthetase (ACS), namely acetyl coenzyme A synthetase, is often used in biochemical research. Acyl coenzyme A synthetase can catalyze the activation of fatty acids by coenzyme A through a two-step thioesterification reaction to produce acyl coenzyme A, and then participate in a variety of anabolic and catabolic lipid metabolism pathways, and participate in the TCA cycle in aerobic respiration.

D-Tagatose (D-(-)-Tagatose) is a natural low-calorie rare sugar. D-Tagatose inhibits the activities of sucrase, maltase and intestinal disaccharidases, reduces the digestion of sucrose and starch, and blocks the absorption of sucrose, maltose and glucose. D-Tagatose promotes glucokinase activity and inhibits glycogen phosphorylase activity via tagatose-1-phosphate, regulates the synthesis and decomposition of hepatic glycogen, reduces postprandial and fasting blood glucose levels, and improves hyperinsulinemia. D-Tagatose regulates lipid profiles, stimulates GLP-1 secretion, and exhibits prebiotic effects. D-Tagatose is a bulking sweetener. D-Tagatose can be used in research related to diabetes, hyperlipidemia, dental caries, atherosclerosis and type 2 diabetes.

Ziltivekimab (COR-001) is a fully human monoclonal antibody and also an IL-6 inhibitor. Ziltivekimab significantly reduces inflammatory biomarkers and Lipoprotein (a) in chronic kidney disease patients with systemic inflammation. Ziltivekimab does not increase pro-atherosclerotic lipid levels. Ziltivekimab is used in studies related to atherosclerotic thrombotic diseases and chronic kidney disease.

Gocdacimab (MEDI6570) is a fully human IgG1 monoclonal antibody inhibitor targeting the lectin-like oxidized low-density lipoprotein receptor LOX-1. By binding to LOX-1 and blocking its function, gocdacimab effectively reduces the level of free soluble LOX-1, thereby inhibiting key pathological processes such as lipid accumulation, foam cell formation, and vascular wall inflammation. Gocdacimab can interfere with atherosclerosis-related mechanisms, and it is used for research on atherosclerosis, and type 2 diabetes mellitus.

Sulfo-Cy5 azide is a near-infrared fluorescent probe with favorable click chemistry reactivity. Sulfo-Cy5 azide enables fluorescence imaging, tissue and cellular visualization of PD-L1 in tumors, and site-specific modification of anti-PD-L1 antibodies. Sulfo-Cy5 azide has been employed for RNA labeling and imaging. Sulfo-Cy5 azide can be conjugated to targeting agents for fluorescence imaging in atherosclerosis and breast cancer models (Ex/Em = 645/670 nm).